title: Antimicrobial and antiurease activities of newly synthesized morpholine derivatives containing an azole nucleus.
abstract: 2-[6-(Morpholin-4-yl)pyridin-3-ylamino]acetohydrazide (4) was obtained starting from 6-morpholin-4-ylpyridin-3-amine (2) via the formation of ester (3) and then converted to the corresponding Schiff bases (5, 6) with the reaction with aromatic aldehydes. The carbothioamide (9), obtained from the reaction of hydrazide with phenylisothiocyanate, was converted to the corresponding 1,2,4-triazole (11) and 1,3,4-thiadiazole (12) derivatives by the treatment with NaOH or H2SO4, respectively. The cyclocondenzation of9with 4-chlorophenacyl bromide or ethyl bromoacetate produced the corresponding 1,3-thiazole (10) or 1,3-thiazolidine derivatives (13), respectively. Antimicrobial and antiurease activities of newly synthesized compounds were investigated. Some of them were found to be active onM. smegmatis, and they displayed activity towardC. albicansandS. cerevisiaein high concentration. Compound10proved to be the most potent showing an enzyme inhibition activity with an IC50= 2.37 ± 0.19 μM.
authors.affiliation: Department of Chemistry, Faculty of Arts and Sciences, Giresun University, 28049 Giresun, Turkey.
authors.forename: Hakan
authors.initials: H
authors.lastname: Bektaş
authors.forename: Sule
authors.initials: S
authors.lastname: Ceylan
authors.forename: Neslihan
authors.initials: N
authors.lastname: Demirbaş
authors.forename: Sengül
authors.initials: S
authors.lastname: Alpay-Karaoğlu
authors.forename: Bahar Bilgin
authors.initials: BB
authors.lastname: Sökmen
keywords: 1,2,4-Triazole; 1,3,4-Oxadiazole; Antimicrobial activity; Antiurease activity; Mannich base; Morpholine